Drug Information

   



      
















Pharmacokinetics


Pyrazinamide is readily
absorbed from the gastrointestinal tract. Peak serum concentrations
occur about 2 hours after a dose by mouth and have been reported to be
about 35 micrograms per mL after 1.5 g, and 66 micrograms per mL after 3
g. Pyrazinamide is widely distributed in body fluids and tissues and
diffuses into the CSF. The half-life has been reported to be about 9 to
10 hours. It is metabolised primarily in the liver by hydrolysis to the
major active metabolite pyrazinoic acid which is subsequently
hydroxylated to the major excretory product 5-hydroxypyrazinoic acid. It
is excreted through the kidney mainly by glomerular filtration. About
70% of a dose appears in the urine within 24 hours mainly as metabolites
and 4 to 14% as unchanged drug. Pyrazinamide is removed by dialysis.
Pyrazinamide is distributed into breast milk.

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Indication
& Dosage




Oral

TUBERCULOSIS: As part of multi-dose regimes during the first two months.
May be continued if necessary into continuation phase also. Adults:
20-35mg/kg/day as a single dose. Dialy max 3g. Intermittent therapy:
50mg/kg thrice a week or 75mg/kg twice a week. One scheme is





Body wt. Daily Thrice weekly Twice Weekly
under 50 kg 1.5g 2.0g 3.0g
over 50 kg 2.0g 2.5g 3.5g

Children: 15-30mg/kg as a single dose. Max 2g daily.

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Action



Bactericidal action against M. tuberculosis in acid
environment present in macrophages and inflammed tissue. Together with
rifampicin provides greatest sterilising action with reduction in
relapse rate. Reduces tubular secretionof uric acid.

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Interaction

Uricosurics: Antagonism of effect of probencid and
sulphinpyrazone.

INH: Significantly reduces INH serum concentration.

Anti-diabetic agents: Affects control of diabetes in diabetics.

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Adverse Effect & Precautions





Nausea, vomiting, myalgia, arthralgia hyperuricaemia and hepatotoxicity.
Rarely hypersensitivity reactions.



Precaution: Periodic liver function test and serum uric acid levels,
diabetes mellitus.

Pregnancy: To given only if clearly needed.

Breast Feeding: Use with caution.

Man: May be used with caution.

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Brands
available in market

















































CAVIZIDE

Merind
TAB 500mg 10 31.00
TAB 750mg 10 46.00
COPYRAZIN

PCI
TAB 500mg 10 37.60
TAB 750mg 10 55.05
TAB 1000mg 10 72.10
TAB 1500mg 10 96.85
MACROZIDE

Macleods
TAB 500mg 10 33.10
TAB 750mg 10 52.00
TAB 1gm 10 68.65
TAB 1.5g 10 95.50
MONTOZIN

Plethico
TAB 500mg 10 17.12
TAB 750mg 10 52.50
P-ZIDE

Cadila Pharma
TAB 500mg 10 33.59
TAB 750mg 10 49.85
TAB 1gm 10 68.65
PYZINA

Lupin
DIS-TAB 300mg 10 26.17
TAB 500mg 10 33.59
TAB 750mg 10 49.50
TAB 1gm 10 65.68
PZA-CIBA

Novartis
TAB 500mg 10×10 335.90
TAB 750mg 10×10 498.50
SYRUP 250mg/5ml 100ml 39.75
TAB 1g 10×10 639.00
PZA-CIBA DISPED

Novartis
DIS TAB 250mg 10×10 0.00
RIZAP

Glaxo
TAB 750mg 10 26.76
TAB 1000mg 10 35.42
TIBIMIDE

Themis pharma
TAB 500mg 10 20.47
TAB 750mg 10 30.45



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Drug Information
   

      

Pharmacokinetics

Pyrazinamide is readily absorbed from the gastrointestinal tract. Peak serum concentrations occur about 2 hours after a dose by mouth and have been reported to be about 35 micrograms per mL after 1.5 g, and 66 micrograms per mL after 3 g. Pyrazinamide is widely distributed in body fluids and tissues and diffuses into the CSF. The half-life has been reported to be about 9 to 10 hours. It is metabolised primarily in the liver by hydrolysis to the major active metabolite pyrazinoic acid which is subsequently hydroxylated to the major excretory product 5-hydroxypyrazinoic acid. It is excreted through the kidney mainly by glomerular filtration. About 70% of a dose appears in the urine within 24 hours mainly as metabolites and 4 to 14% as unchanged drug. Pyrazinamide is removed by dialysis. Pyrazinamide is distributed into breast milk.

Top
   

Indication & Dosage

Oral
TUBERCULOSIS: As part of multi-dose regimes during the first two months. May be continued if necessary into continuation phase also. Adults: 20-35mg/kg/day as a single dose. Dialy max 3g. Intermittent therapy: 50mg/kg thrice a week or 75mg/kg twice a week. One scheme is

Body wt.

Daily

Thrice weekly

Twice Weekly

under 50 kg

1.5g

2.0g

3.0g

over 50 kg

2.0g

2.5g

3.5g

Children: 15-30mg/kg as a single dose. Max 2g daily.

Top
   

Action

Bactericidal action against M. tuberculosis in acid environment present in macrophages and inflammed tissue. Together with rifampicin provides greatest sterilising action with reduction in relapse rate. Reduces tubular secretionof uric acid.

Top
   

Interaction

Uricosurics: Antagonism of effect of probencid and sulphinpyrazone.
INH: Significantly reduces INH serum concentration.
Anti-diabetic agents: Affects control of diabetes in diabetics.

Top
   

Adverse Effect & Precautions

Nausea, vomiting, myalgia, arthralgia hyperuricaemia and hepatotoxicity. Rarely hypersensitivity reactions.

Precaution: Periodic liver function test and serum uric acid levels, diabetes mellitus.
Pregnancy: To given only if clearly needed.
Breast Feeding: Use with caution.
Man: May be used with caution.

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CAVIZIDE

Merind

TAB

500mg

10

31.00

TAB

750mg

10

46.00

COPYRAZIN

PCI

TAB

500mg

10

37.60

TAB

750mg

10

55.05

TAB

1000mg

10

72.10

TAB

1500mg

10

96.85

MACROZIDE

Macleods

TAB

500mg

10

33.10

TAB

750mg

10

52.00

TAB

1gm

10

68.65

TAB

1.5g

10

95.50

MONTOZIN

Plethico

TAB

500mg

10

17.12

TAB

750mg

10

52.50

P-ZIDE

Cadila Pharma

TAB

500mg

10

33.59

TAB

750mg

10

49.85

TAB

1gm

10

68.65

PYZINA

Lupin

DIS-TAB

300mg

10

26.17

TAB

500mg

10

33.59

TAB

750mg

10

49.50

TAB

1gm

10

65.68

PZA-CIBA

Novartis

TAB

500mg

10×10

335.90

TAB

750mg

10×10

498.50

SYRUP

250mg/5ml

100ml

39.75

TAB

1g

10×10

639.00

PZA-CIBA DISPED

Novartis

DIS TAB

250mg

10×10

0.00

RIZAP

Glaxo

TAB

750mg

10

26.76

TAB

1000mg

10

35.42

TIBIMIDE

Themis pharma

TAB

500mg

10

20.47

TAB

750mg

10

30.45

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By |2022-07-20T16:45:00+00:00July 20, 2022|Uncategorized|Comments Off on Pyrazinamide

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